CA2600832C - Inhibiteurs de l'integrase du vih - Google Patents

Inhibiteurs de l'integrase du vih Download PDF

Info

Publication number
CA2600832C
CA2600832C CA2600832A CA2600832A CA2600832C CA 2600832 C CA2600832 C CA 2600832C CA 2600832 A CA2600832 A CA 2600832A CA 2600832 A CA2600832 A CA 2600832A CA 2600832 C CA2600832 C CA 2600832C
Authority
CA
Canada
Prior art keywords
oxo
hydroxy
fluorobenzyl
methyl
carboxamide
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2600832A
Other languages
English (en)
Other versions
CA2600832A1 (fr
Inventor
Giuseppe Cecere
Maria Del Rosario Rico Ferreira
Philip Jones
Paola Pace
Alessia Petrocchi
Vincenzo Summa
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
MSD Italia SRL
Original Assignee
Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Istituto di Ricerche di Biologia Molecolare P Angeletti SpA filed Critical Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Publication of CA2600832A1 publication Critical patent/CA2600832A1/fr
Application granted granted Critical
Publication of CA2600832C publication Critical patent/CA2600832C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2600832A 2005-03-31 2006-03-22 Inhibiteurs de l'integrase du vih Expired - Fee Related CA2600832C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US66689705P 2005-03-31 2005-03-31
US60/666,897 2005-03-31
PCT/GB2006/001062 WO2006103399A1 (fr) 2005-03-31 2006-03-22 Inhibiteurs de l’integrase du vih

Publications (2)

Publication Number Publication Date
CA2600832A1 CA2600832A1 (fr) 2006-10-05
CA2600832C true CA2600832C (fr) 2011-12-13

Family

ID=36648790

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2600832A Expired - Fee Related CA2600832C (fr) 2005-03-31 2006-03-22 Inhibiteurs de l'integrase du vih

Country Status (7)

Country Link
US (2) US7981879B2 (fr)
EP (1) EP1866313A1 (fr)
JP (1) JP5116660B2 (fr)
CN (1) CN101146811B (fr)
AU (1) AU2006228278C1 (fr)
CA (1) CA2600832C (fr)
WO (1) WO2006103399A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8377960B2 (en) 2007-11-15 2013-02-19 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7273859B2 (en) * 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
US7491819B1 (en) 2004-05-28 2009-02-17 Bristol-Myers Squibb Company N-[4-Fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide as an HIV integrase inhibitor
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7192948B2 (en) * 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
KR101363875B1 (ko) 2005-04-28 2014-02-21 시오노기세야쿠 가부시키가이샤 Ｈｉｖ 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체
US7494984B2 (en) 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
US7897592B2 (en) 2005-11-15 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7902182B2 (en) 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
US8039458B2 (en) * 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007143446A1 (fr) 2006-05-30 2007-12-13 Bristol-Myers Squibb Company Composés hétérotricycliques spiro-condensés utilisés en tant qu'inhibiteurs de la vih intégrase
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
JP5208962B2 (ja) 2006-12-22 2013-06-12 アベキサ・リミテッド 二環式ピリミジノンおよびその使用
US7763630B2 (en) 2007-06-06 2010-07-27 Bristol-Myers Squibb Company HIV integrase inhibitors
ES2402322T3 (es) * 2007-11-15 2013-04-30 Gilead Sciences, Inc. Inhibidores de la replicación del virus de la inmunodeficiencia humana
EA019259B1 (ru) 2007-11-16 2014-02-28 Джилид Сайенсиз, Инк. Ингибиторы репликации вируса иммунодефицита человека
US8129398B2 (en) * 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
JP5592360B2 (ja) * 2008-07-02 2014-09-17 アベキサ・リミテッド イミダゾピリミジノンおよびその使用
WO2010042391A2 (fr) * 2008-10-06 2010-04-15 Merck Sharp & Dohme Corp. Inhibiteurs de l'intégrase du vih
JP2012516333A (ja) * 2009-01-28 2012-07-19 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラーゼ阻害剤としての架橋化合物
US8143244B2 (en) 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
WO2011025683A1 (fr) * 2009-08-26 2011-03-03 Merck Sharp & Dohme Corp. Inhibiteurs de l'intégrase du vih
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
WO2012009446A1 (fr) 2010-07-16 2012-01-19 Concert Pharmaceuticals Inc. Nouveaux dérivés pyrimidinecarboxamide
CN102336751A (zh) * 2010-07-16 2012-02-01 爱维艾珂瑟有限公司 新型抗病毒剂
US9013997B2 (en) 2012-06-01 2015-04-21 Broadcom Corporation System for performing distributed data cut-through
WO2014008636A1 (fr) * 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Composés macrocycliques en tant qu'inhibiteurs de l'intégrase du vih
EP2931730B1 (fr) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. Dérivés 4-pyridinonetriazines en tant qu'inhibiteurs de l'intégrase du vih
US9493479B2 (en) 2013-04-16 2016-11-15 Merck Sharp & Dohme Corp. Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
RS56701B1 (sr) 2013-05-17 2018-03-30 Merck Sharp & Dohme Fuzionisana triciklična heterociklična jedinjenja kao inhibitori hiv integraze
EP3008044B1 (fr) 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Composés hétérocycliques tricycliques fusionnés utiles en tant qu'inhibiteurs de l'intégrase du vih
UA117499C2 (uk) 2013-09-27 2018-08-10 Мерк Шарп Енд Доум Корп. Заміщені похідні хінолізину, які можна використовувати як інгібітори інтегрази віл
GB201322334D0 (en) 2013-12-17 2014-01-29 Agency Science Tech & Res Maleimide derivatives as modulators of WNT pathway
WO2015089847A1 (fr) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Composés à hétérocycles spirocycliques utiles en tant qu'inhibiteurs d'intégrase du vih
WO2016187788A1 (fr) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Composés hétérocycliques tricycliques fusionnés utiles pour traiter l'infection au vih
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
US10544155B2 (en) 2015-12-15 2020-01-28 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as HIV integrase inhibitors
CN105523998B (zh) * 2015-12-16 2019-12-17 杨冰 一种甲巯咪唑的制备工艺
WO2017113288A1 (fr) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Composés hétérocycliques tricycliques condensés utiles en tant qu'inhibiteurs de l'intégrase du vih
CA3042314A1 (fr) 2016-12-02 2018-06-07 Merck Sharp & Dohme Corp. Composes heterocycliques tricycliques utiles en tant qu'inhibiteurs de l'integrase du vih
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
EP3573984A4 (fr) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. Dérivés de quinolizine substitués utiles en tant qu'inhibiteurs de l'intégrase du vih
MY201239A (en) 2019-03-22 2024-02-13 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
PE20221569A1 (es) 2020-02-24 2022-10-06 Gilead Sciences Inc Compuestos tetraciclicos para el tratamiento de infecciones por vih
ES3064867T3 (en) 2020-09-30 2026-04-29 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds for a use in the treatment of hiv
US11613546B2 (en) 2021-01-19 2023-03-28 Gilead Sciences, Inc. Substituted pyridotriazine compounds and uses thereof
TW202446773A (zh) 2022-04-06 2024-12-01 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262055B1 (en) 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
US6380249B1 (en) 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6306891B1 (en) 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
AU5880600A (en) 1999-06-25 2001-01-31 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
WO2002036734A2 (fr) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza- et polyaza-naphtalenyl cetones utiles en tant qu'inhibiteurs de l'integrase du vih
EP1326611B1 (fr) 2000-10-12 2007-06-13 Merck & Co., Inc. Azanaphthalenylcarboxamides et polyazanaphthalenylcarboxamides utiles en tant qu'inhibiteurs de la vih integrase
PL360944A1 (en) 2000-10-12 2004-09-20 Merck & Co, Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
ATE345129T1 (de) 2000-10-12 2006-12-15 Merck & Co Inc Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
ES2572030T3 (es) 2001-08-10 2017-07-19 Shionogi & Co., Ltd. Agente antiviral
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
EP1467970B1 (fr) 2002-01-17 2007-08-22 Merck & Co., Inc. Carboxamides hydroxynaphthyridinone utiles comme inhibiteurs de l'integrase du vih
NZ540729A (en) 2002-12-27 2008-03-28 Angeletti P Ist Richerche Bio Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors
WO2004062613A2 (fr) 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Inhibiteurs d'integrase hiv
US7037908B2 (en) 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors
US20040229982A1 (en) * 2003-05-14 2004-11-18 Goossens Danielle F. Stabilized flame retardant additives and their use
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
US7176196B2 (en) * 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7192948B2 (en) 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7173022B2 (en) 2004-05-28 2007-02-06 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7157447B2 (en) 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7491819B1 (en) 2004-05-28 2009-02-17 Bristol-Myers Squibb Company N-[4-Fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide as an HIV integrase inhibitor
WO2007064316A1 (fr) 2005-11-30 2007-06-07 Bristol-Myers Squibb Company Heterocycles bicycliques en tant qu'inhibiteurs de l'integrase du vih

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8377960B2 (en) 2007-11-15 2013-02-19 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication

Also Published As

Publication number Publication date
CN101146811A (zh) 2008-03-19
JP2008534561A (ja) 2008-08-28
WO2006103399A8 (fr) 2007-11-01
AU2006228278B2 (en) 2010-07-22
US20110257162A1 (en) 2011-10-20
US7981879B2 (en) 2011-07-19
AU2006228278C1 (en) 2011-06-23
EP1866313A1 (fr) 2007-12-19
US20090253681A1 (en) 2009-10-08
CN101146811B (zh) 2012-01-11
WO2006103399A1 (fr) 2006-10-05
AU2006228278A1 (en) 2006-10-05
CA2600832A1 (fr) 2006-10-05
JP5116660B2 (ja) 2013-01-09

Similar Documents

Publication Publication Date Title
CA2600832C (fr) Inhibiteurs de l'integrase du vih
AU2003292436B2 (en) Tetrahydro-4H-pyrido[1,2-A]pyrimidines and related compounds useful as HIV integrase inhibitors
EP2456774B1 (fr) Dérivés condensés d'aminodihydro-oxazine
US7348425B2 (en) Inhibitors of HCV replication
TWI385175B (zh) 作為β-分泌酶調節劑之螺旋-三環化合物及其使用方法
US20060046983A1 (en) Inhibitors of HCV replication
AU2023368731A1 (en) Nitrogen-containing fused ring compound, intermediate thereof, preparation method therefor and use thereof
PT2989106T (pt) Compostos heterocíclicos fundidos como inibidores da proteína quinase
PT1910348T (pt) Compostos de benzotiazol e azabenzotiazol úteis como inibidores de quinases
AU2006276231A1 (en) HIV reverse transcriptase inhibitors
EP1725102A1 (fr) Inhibiteurs de l'integrase du vih
WO2018118829A1 (fr) Composés hétérocycliques en tant qu'inhibiteurs de la protéase du vih
BR112020008121A2 (pt) compostos espirocíclico de alqueno como moduladores de receptor farnesoide x
CN121548418A (zh) 二环杂芳基化合物
WO2009154870A1 (fr) Inhibiteurs de l'intégrase vih
CA2568389A1 (fr) Inhibiteurs integrase vih
CA2542047A1 (fr) Composes pyridopyrrolopyrazine dione hydroxy utiles comme inhibiteurs de l'integrase du vih
CA3176635A1 (fr) 1,4-diazepanones bicycliques et leurs utilisations therapeutiques
RU2169148C2 (ru) АНЕЛЛИРОВАННЫЕ β--КАРБОЛИНЫ
MXPA06010252A (en) Hiv integrase inhibitors

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed

Effective date: 20160322